Gohel M C, Patel T M, Parikh R K, Parejiya P B, Barot B S, Ramkishan A
Lallubhai Motilal College of Pharmacy, Navarangpura, Ahmedabad-380 009, India.
Indian J Pharm Sci. 2012 Sep;74(5):381-6. doi: 10.4103/0250-474X.108412.
The aim of this investigation was to develop a novel multifunctional co-processed diluent consisting of microcrystalline cellulose (Avicel PH 102), crospovidone (Polyplasdone XL) and polyethylene glycol 4000. Colloidal silicon dioxide and talc were also incorporated as minor components in the diluent to improve tableting properties. Melt granulation was adopted for preparation of co-processed diluent. Percentage of Avicel PH 102, Polyplasdone XL and polyethylene glycol 4000 were selected as independent variables and disintegration time was chosen as a dependent variable in simplex lattice design. The co-processed diluent was characterised for angle of repose, bulk density, tapped density, Carr's index, percentage of fines and dilution potential study. Acetaminophen and metformin were used as poorly compressible model drugs for preparation of tablets. The blend of granules of drug and extra-granular co-processed diluent exhibited better flow as compared to the blend of drug granules and physical mixture of diluents blend. The diluent exhibited satisfactory tableting properties. The tablets exhibited fairly rapid drug release. In conclusion, melt granulation is proposed as a method of preparing co-processed diluent. The concept can be used to bypass patents on excipient manufacturing.
本研究的目的是开发一种新型多功能共处理稀释剂，其由微晶纤维素（Avicel PH 102）、交联聚维酮（Polyplasdone XL）和聚乙二醇4000组成。胶态二氧化硅和滑石粉也作为次要成分加入到稀释剂中以改善压片性能。采用熔融制粒法制备共处理稀释剂。在单纯形格子设计中，选择Avicel PH 102、Polyplasdone XL和聚乙二醇4000的百分比作为自变量，崩解时间作为因变量。对共处理稀释剂进行休止角、堆密度、振实密度、卡尔指数、细粉百分比和稀释潜力研究等特性表征。对乙酰氨基酚和二甲双胍用作难压缩模型药物来制备片剂。与药物颗粒和稀释剂物理混合物的混合物相比，药物颗粒与颗粒外共处理稀释剂的颗粒混合物表现出更好的流动性。该稀释剂表现出令人满意的压片性能。片剂表现出相当快速的药物释放。总之，建议采用熔融制粒法制备共处理稀释剂。该概念可用于规避辅料制造方面的专利。
